Aliskiren (CGP 60536; CGP60536B; SPP 100) hydrochloride 是一种口服有效的、选择性的肾素 (renin) 抑制剂，IC50为 1.5 nM。Aliskiren hydrochloride 可用于高血压、心血管疾病和癌症恶病质的研究。
| 生物活性 | Aliskiren (CGP 60536; CGP60536B; SPP 100) hydrochloride is an orally active and selectiverenininhibitor, withIC50of 1.5 nM. Aliskiren hydrochloride can be used for the research of hypertension, cardiovascular diseases andcancercachexia[1]-[4]. |
| IC50& Target | IC50: 1.5 nM (renin)[1]; 0.6 nM (human renin), 2 nM (marmoset renin), 80 nM (rat renin), 7 nM (dog renin), 11 nM (rabbit renin), 63 nM (guinea pig renin), 150 nM (pig renin)[2] |
体外研究
(In Vitro) | Aliskiren hydrochloride inhibits plasma renin activity (PRA) in vitro with IC50s of 2.9 nM (human PRA), 8.0 nM (monkey PRA), respectively[1].
Aliskiren hydrochloride (10 μM; 24 h) inhibits prorenin-induced human aortic smooth muscle cell migration[2].
Aliskiren hydrochloride (1-10 μM; 24 h) inhibits both the lamellipodia formation and morphological changes induced by prorenin with no significant effect on PDGF-BB activity[2].
Cell Migration Assay[2] | Cell Line: | Smooth muscle cell (SMC) | | Concentration: | 1-10 μM | | Incubation Time: | 24 hours | | Result: | Inhibited human aortic smooth muscle cell migration induced by prorenin (10 nM) at 10 μM. |
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体内研究
(In Vivo) | Aliskiren hydrochloride (3 mg/kg, 10 mg/kg; p.o.; daily; 0-12 d) inhibit renin and lower blood pressure without affecting heart rate in sodium-depleted marmosets[3].
Aliskiren hydrochloride (10 mg/kg; p.o.; single dose) delays cachexia development, reduces tumor, and prolongs mouse survival. And also improves whole-body strength, mobility and coordination, enhances locomotor activity, and inhibits muscle wasting[4].
Aliskiren hydrochloride (10 mg/kg; p.o.; single dose; 20 d after C26 injection) reduces oxidative stress associated with cancer cachexia[4].
| Animal Model: | Sodium-depleted marmosets[3] | | Dosage: | 3 mg/kg, 10 mg/kg | | Administration: | Oral gavage; once daily; 12 days | | Result: | Increased plasma immunoreactive renin levels, and lowered blood pressure without affecting heart rate.
Showed no rebound increase in BP following the end of treatment with either dose of aliskiren.
Inhibited the RAS and controls the upregulation of pro-inflammatory cytokines. |
| Animal Model: | Cancer cachexia model in BALB/c mice injected with C26 mouse colon carcinoma cells[4] | | Dosage: | 10 mg/kg | | Administration: | Oral gavage; on day 5 (as a preventive strategy, AP group) or on day 12 (as a therapeutic strategy, AT group) after C26 injection; for 20 days after C26 injection | | Result: | Enhanced grip strength, coordination, and locomotor activity.
Inhibited serum Ang I and Ⅱ levels and both serum and muscular tumor necrosis factor-α (TNF-α) and inter- leukin-6 (IL-6) levels. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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